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Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Stewart AO, Cowart MD, Moreland RB, Latshaw SP, Matulenko MA, Bhatia PA, Wang X, Daanen JF, Nelson SL, Terranova MA, Namovic MT, Donnelly-Roberts DL, Miller LN, Nakane M, Sullivan JP, Brioni JD. Stewart AO, et al. J Med Chem. 2004 Apr 22;47(9):2348-55. doi: 10.1021/jm0305669. J Med Chem. 2004. PMID: 15084133
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Zheng GZ, Bhatia P, Kolasa T, Patel M, El Kouhen OF, Chang R, Uchic ME, Miller L, Baker S, Lehto SG, Honore P, Wetter JM, Marsh KC, Moreland RB, Brioni JD, Stewart AO. Zheng GZ, et al. Among authors: stewart ao. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4936-40. doi: 10.1016/j.bmcl.2006.06.053. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16809035
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Kolasa T, Matulenko MA, Hakeem AA, Patel MV, Mortell K, Bhatia P, Henry R, Nakane M, Hsieh GC, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino B, El Kouhen O, Marsh KC, Wetter JM, Moreland RB, Brioni JD, Stewart AO. Kolasa T, et al. Among authors: stewart ao. J Med Chem. 2006 Aug 24;49(17):5093-109. doi: 10.1021/jm060279f. J Med Chem. 2006. PMID: 16913699
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO. Patel MV, et al. Among authors: stewart ao. J Med Chem. 2006 Dec 14;49(25):7450-65. doi: 10.1021/jm060662k. J Med Chem. 2006. PMID: 17149874
53 results